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| United States Patent |
6,183,758
|
|
Scott
|
February 6, 2001
|
Phytochemicals, nutrients & medication absorption &/or treatment
Abstract
A skin absorbent cream including the ingredients MSM, urea, propylene
glycol and a large molecular medication. This combination of ingredients
softens the skin to allow penetration of the medication through the skin
and into the underlying blood vessels. The large molecular medication
dissolves in the propylene glycol between as low as 25.degree. C. to
150.degree. C. and becomes the transporter through the outer skin layer
and into the blood stream.
| Inventors:
|
Scott; Kenneth Duane (Scotts Mills, OR)
|
| Assignee:
|
Highland Laboratories, Inc. (Mt. Angel, OR)
|
| Appl. No.:
|
015351 |
| Filed:
|
January 29, 1998 |
| Current U.S. Class: |
424/401; 514/844; 514/944 |
| Intern'l Class: |
A61K 031/74; A61K 006/00; A61K 007/00 |
| Field of Search: |
424/78.02,78.03,401
514/937,944,946,947,844
|
References Cited
U.S. Patent Documents
| 4477469 | Oct., 1984 | Herschler | 424/322.
|
| 5874074 | Feb., 1999 | Smith | 424/78.
|
Other References
Article entitled "Skin Penetration Enhancers Cited in the Technical
Literature" from Pharmaceutical Technology, Nov., 1997.
Article entitled "Advances in Drug Delivery" from Pharmaceutical
Technology, Jan., 1998.
"Percutaneous Absorption" from 14th Ed. Remington's Pharmaceutical Science.
|
Primary Examiner: Page; Thurman K.
Assistant Examiner: Howard; S.
Attorney, Agent or Firm: Harrington; Robert L.
Claims
What is claimed is:
1. A composition for penetrating through the skin to underlying blood
vessels consisting essentially of methyl sulfonyl methane urea, propylene
glycol and an organic compound having structure, function or medicinal
properties.
2. A composition for penetrating through the skin and into underlying blood
vessels consisting essentially of:
(a) a mixture of methly sulfonyl methane and urea dissolved in purified
water;
(b) a mixture of a quantity of propylene glycol and a quantity of an
organic compound having structure, function or medicinal properties
dissolved in the propylene glycol; and
(c) said mixture of compound (a) blended with said mixture of compound (b).
3. An emulsion or gel that forms a base cream or gel and the composition of
claim 1 mixed into the base cream or gel to form a medicinal, structure or
function cream or gel.
4. A composition as defined in claim 2 wherein substantially equal parts
plus or minus 50% of propylene glycol, urea, and methyl sulfonyl methane
are mixed with a quantity of the organic compound totally dissolved in the
propylene glycol, the organic compound being about 20% of the propylene
glycol.
5. A composition as defined in claim 2 wherein the large molecular organic
compound is either a steroid, alkaloid or nutrient.
6. A process for producing a composition for penetrating through the skin
and into the blood vessels which consisting essentially of:
(a) producing a dissolved mixture of urea and methyl sulfonyl methane;
(b) producing a dissolved mixture of propylene glycol with a large
molecular organic substance; and
(c) inter-mixing ingredients (a) and (b).
7. A process as defined in claim 6 wherein the propylene glycol is heated
to a temperature between 25.degree. C. and 150.degree. C. and completely
dissolving the organic substance therein prior to inter-mixing with the
dissolved compound in step (a).
8. A process for producing skin penetrating medicinal treatment or to
assist in the structure or function substance which includes:
producing an emulsion or a gel suitable as a skin cream or gel and adding
thereto the substance of claim 7.
Description
FIELD OF THE INVENTION
This invention relates to the phytochemical, nutrient & medication for
improved structure, function &/or treatment of specific conditions in
humans and animals through the process of skin penetration, and more
particularly it relates to a skin ointment with improved skin penetration
properties.
BACKGROUND OF THE INVENTION
Phytochemicals, nutrients & medications intended for transmission via the
blood stream are typically entered into a person's blood stream through
oral ingestion or syringe injection. An alternative form of treatment is
the application of the phytochemicals, nutrients or medications to the
skin with the medication being absorbed through the skin into the blood
vessels underlying the epidermis part of the skin.
There are advantages of the skin application technique, i.e. the compounds
can be applied to the place of the needed improvement of the structure,
function or ailment and absorption into the blood vessels surrounding this
condition provides a more direct and often a more effective
treatment/repair of the structure, function or ailment. The problem with
the technique is achieving penetration of the skin and specifically the
stratum corneum area of the skin.
The compounds themselves are often not skin absorbable (evidence shows the
only possible exceptions to this are sodium ions and water) and must be
dissolved into a carrier or transport solution. There are solutions that
can be made to be somewhat skin absorbent, especially when they are
applied and then covered with a barrier such as plastic (example is Dow's
Saran wrap) and this causes water to travel in and out of this upper layer
of skin. This system is limited to "patches" already prepared, is
expensive and limits the amount of ingredient that can be applied and the
physical area that the plastic patch can be applied. Solvents are known
that will achieve this in the presence of a "patch" but they must be at a
precise ratio of ingredient to the solvent (near saturation point). Known
solutions that are acceptable for topical application and used without a
"patch" are either not sufficiently absorbable into the skin or not
sufficiently solvent, e.g., if the ingredient is one having large
molecules, the solution does not readily dissolve the medication.
SUMMARY OF THE INVENTION
The present invention involves the combination of two separate and
seemingly unrelated solutions. The first solution has a makeup of water,
methyl sulfonyl methane (MSM--the oxide form of DMSO) and urea. MSM & urea
in combination produce some but no significant penetration of the skin and
they do not dissolve the large molecules often found in phytochemicals
(active plant compounds), organic nutrients or prescribed medications. The
combination of MSM and urea, used topically, is itself patented (U.S. Pat.
No. 4,477,469) and has a number of benefits. One not so well known or
appreciated is its ability not only to "soften" the skin but actually open
the "horny layer" (stratum corneum, stratum lucidum & stratum granulosum)
to allow penetration of water and organic solvents such as propylene
glycol.
The second solution includes as one of the ingredients propylene glycol.
Propylene glycol is recognized as being beneficial for skin penetration
and it dissolves large molecules, e.g., at temperatures of between about
25.degree. and 150.degree. C. However, in the past to get the large
organic molecules to pass the horny layer and be released one had to use a
minimum amount of propylene glycol to solublize the compound and cover the
area with the before mentioned "patch". In this current invention it has
been found that the before mentioned limits do not apply. Therefore with
this second solution the desired ingredient (phytochemical, nutrient or
medication) is dissolved in the propylene glycol completely and without
being at the saturation point.
Upon mixing the two solutions, the mixture surprisingly produces rapid
penetration of the ingredient through the skin tissue (epidermis) and into
the blood vessels underlying the skin tissue (the dermis & subcutaneous
tissues). It is theorized that the MSM & urea, although only a mediocre
skin penetration, expands the platelets of the skin particularly in the
horny layer of the skin. The expansion of the platelets opens the
interstices and enables the rapid penetration of the propylene glycol
solution, i.e., containing the active compound (phytochemical, nutrient or
medication).
The invention will be more fully appreciated upon reference to the
following detailed description of a preferred embodiment of the invention
having reference to the accompanying drawings.
BRIEF DESCRIPTION OF THE FIGURES
FIG. 1 is a schematic illustration of human skin; and
FIGS. 2A-2D are schematic illustrations of a process used for producing an
ointment of the present invention.
DESCRIPTION OF THE PREFERRED EMBODIMENT
The present invention relates to the medicinal, structure or function
treatment of a human or animal. Illustrated is a person's skin layer 10.
It will be understood that the invention here is transportation of the
medication, nutrient or phytochemical into a person's blood stream through
the skin tissue. There are many conditions, some that are localized and
will be more directly benefitted by the invention herein but others that
are not localized which nevertheless will benefit from the medication,
nutrient or phytochemical introduced into the blood stream. The invention
provides the form of delivery which is here referred to as skin
absorption.
Oral injection is a common alternative form but is not always desirable to
the individual and the beneficial effects are slower and the
gastrointestinal tract may either inhibit or destroy certain compounds.
Syringe induction is a further alternative form and produces quick results
but is often not desirable to the individual.
Patch absorption is limited in active ingredient and due to its nature is
not always desirable and can have poor individual acceptance.
Skin injection through topical application is the least objectionable but
the skin is a very effective barrier to many compounds (other than sodium
and water). A typical skin injection technique is to dissolve the compound
to be used in a liquid transporter or carrier that has the capability of
penetrating or being absorbed by the skin. The process has not gained wide
acceptance for a number of reasons. In some instances there is a concern
for side affects from the transporting substance which is also injected
into the blood stream. Some transporting substances (such as the
Nicotinate salts) have low patient acceptance due to the skin irritation
caused, others may cause other unacceptable side effects. Of those known
to be safe, their absorbent properties are not effectively adequate and/or
they do not dissolve the large molecular compounds contemplated by the
present invention.
Two substances which fit the category of being marginal absorbents are MSM
and urea (in combination) and propylene glycol. MSM and urea (in
combination) is used for a number of different types of medicinal and
nutrient application (internally and topically--see U.S. Pat. No.
4,477,469). As a topical (skin applied) ointment, the MSM-urea is believed
to prevent cross-linking so as to slow the effects of UV light (sunlight)
and thus impedes the aging of skin. It can be observed to soften the skin.
Experiments have shown that the MSM-urea blend will absorb into the outer
layer of the skin but not sufficiently to function as an effective
medicinal or nutrient carrier or transporter.
Propylene glycol is an excellent absorber of large molecular compounds,
e.g., of steroid type medication. However, propylene glycol, like
MSM-urea, will absorb into the skin but again not, by itself, sufficiently
to function as an effective medicinal or nutrient carrier. The combination
of MSM-urea and propylene glycol might be expected to produce an ointment
that dissolves large molecular medications, phytochemicals or nutrients
and inhibit cross-linking, but would not be expected to produce an
effective absorbent of these compounds.
This combination nevertheless does produce an excellent transporter of
large molecular medications (e.g., steroids & alkaloids). It is theorized
that the major inhibitor to the absorption of propylene glycol is the
horny outer layers of skin. It is further theorized that the MSM-urea
functions to swell or expand the platelets in this outer horny skin layer
which opens the interstices between the platelets. This facilitates the
transportation of the propylene glycol (and the medication, phytochemical
or nutrient dissolved therein) through this outer layer and thus enabling
the rapid transportation of the medication into the blood stream.
The procedure just described is illustrated in FIG. 1. Reference number 10
refers to the skin and the layers of skin including the horny outer layer
(stratum corneum) 12 and the underlying layers (stratum lucidum and
stratum granulosum) sometimes referred to as the true skin layer 14 and
the adipose tissue layer (including the dermis and subcutaneous tissue)
16. Imbedded in the adipose layer and the dermis layer are the blood
vessels 18. As will be noted, the horny outer shell is indicated to be
made of overlapping platelets 20 and swelling of the platelets is believed
to open interstices 22 between the platelets 20.
Regardless, the combination has produced an excellent topical ointment for
transportation of large molecular phytochemicals, nutrients and
medications through the skin 10 and into the underlying blood vessels 18.
FIGS. 2A-2D schematically illustrate the process for producing a topical
ointment in accordance with the invention. In FIG. 2A, there is first
mixed the materials of the MSM and urea with purified water. This is
described in detail in U.S. Pat. No. 4,477,469 and the disclosure thereof
is incorporated herein by reference. MSM is available from Vita-Flex
Nutrition, P.O. Box 070140, Staten Island, N.Y. 10307-0140 or Carolwood
Corporation, 305 Third St., Greenville, Pa. 16125. Urea and propylene
glycol (cosmetic grades) are available from numerous sources in the U.S.A.
and as such should cause no problem locating adequate supply.
The mixture of propylene glycol and any large molecular compounds
(phytochemicals, nutrients or medication) is illustrated in FIG. 2B. The
propylene glycol is heated to about 120.degree. C. and the active
ingredient (phytochemical, nutrient or medication) is added. FIG. 2C
represents the inter-mixture of the MSM-urea solution and propylene glycol
solution (with the dissolved ingredient) and FIG. 2D represents the
mixture of FIG. 2C added to an emulsion or gel 24, e.g., any of a number
of creamy or gel substances prepared for topical application including
ointments and salves. The general category of skin creams (or gels) are
considered desirable as they are widely used and accepted for skin health
and beautification.
Whereas the above description is considered to adequately teach a person
skilled in this art how to produce the product of the invention, the
following is a detailed example of the ingredients and procedures.
EXAMPLE
Formulation For Manufacture
Ingredients Amount
FACE CREAM BASE 587.76 GM
GLYCERIN 10.00 GM
VIT E LIQ 1000 IN GRAM 10.00 GM
WATER (Deionized) 99.00 GM
PROPYLENE GLYCOL 100.00 GM
PROGESTERONE POWDER 19.00 GM
UREA 100.00 GM
MSM 70.00 GM
FRAGRANCE 4.00 GM
CITRIC ACID 0.25 GM
The process used to produce the topical ointment from these ingredients
involves (a) heating a mixture of the Vitamin E and glycol to 120 C., (b)
add the progesterone to the mixture, (c) cool the above to 85.degree. C.
and blend it into the cosmetic base cream which is previously warmed to
40.degree. C., (d) add the urea and MSM previously dissolved in most of
the water (heated), (e) the citric acid is dissolved in the remaining
water and cooled to 28.degree. C. or less (stir every 20 minutes), and (f)
blend the citric acid solution and the citrus fragrance into the base
cream mixture and check the acidic (pH) reading to assure that it is
between 5.0 and 5.4.
The above disclosures are by way of example only and those skilled in the
art will appreciate that the invention can be produced in numerous
variations and forms. Accordingly, the invention is not limited by the
disclosures but rather is defined by the claims appended hereto.
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